Zibo Hangyu Biotechnology Development Co., Ltd is a leading manufacturer and supplier of chemicals in China. We develop produce and distribute high quality pharmaceuticals, intermediates, special chemicals and OLED intermediates and other fine chemi
Cas:915087-33-1
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inquiryChemvon Biotechnology is one of the leading high-technology manufacturer in the field of pharmaceutical and fine chemical industry. From origins as a research group in technology service, chemvon has progressed into an integrated company with a
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inquiryProduct Name: Enzalutamide Assay: 99.0% Cas No.: 915087-33-1 Usage:It is used to treat advanced castration-tolerant prostate cancer in men who have spread or relapsed. Appeara
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inquiryShandong Mopai Biotechnology Co., LTD is a leading manufacturer and supplier of chemicals in China. We develop produce and distribute high quality pharmaceuticals, intermediates, special chemicals and OLED intermediates and other fine chemicals. W
Good price, high purity, mature production technology, accept custom synthesis per customer's requirements Appearance:White Solid Package:As per Customer‘ requirements Application:ANTI-CANCER
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inquiryDayangChem exported this product to many countries and regions at best price. If you are looking for the material's manufacturer or supplier in China, DayangChem is your best choice. Pls contact with us freely for getting detailed product spe
Items Standard Test Result Appearance White to off-white crystalline powder Conforms Purity, %
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inquiryhebei yanxi chemical co., LTD who registered capital of 10 million yuan, nearly to $2 million, we have a pharmaceutical raw materials factory production of pharmaceutical raw materials, and a reagent r&d center, and we do research and developm
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inquiry1. Guaranteed purity; 2. Large quantity in stock; 3. Largest manufacturer; 4. Best service after shipment with email; 5. High quality & competitive price; ...... Appearance:White crystalline powder Storage:2-8°C Package:10g/bottle; 10
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inquiryEnzalutamide CAS No.: 915087-33-1 Name: Enzalutamide Synonyms: 4-[3-[4-Cyano-3-(trifluoromethyl)phenyl]-5,5-dimethyl-4-oxo-2-thioxo-1-imidazolidinyl]-2-fluoro-N-methylbenzamide
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inquiry1. Factory price and high quality must be guaranteed, base on 8 years of production and R&D experience2. Free samples will be provided,ensure specifications and quality are right for customer3. Customers will receive the most professional technical s
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inquiryShanghai Seasonsgreen Chemical is a high-tech research and development, production, sale and custom synthesis set in one high-tech chemical products enterprises. Our sales and marketing division is located in Shanghai, serving international pharmaceu
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Product Name: Enzalutamide Synonyms: Enzalutamide (Xtandi);4-{3-[4-CYANO-3-(TRIFLUOROMETHYL)PHENYL]-5,5-DIMETHYL-4-OXO-2-SULFANYLIDENEIMIDAZOLIDIN-1-YL}-2-FLUO;4-(3-(4-Cyano-3-(trifluoromethyl)phenyl)-5,5-dimethyl-4-oxo-2-thioxoimidazolidin-1-yl)-
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inquiryWith our good experience, we offer detailed technical support and advice to assist customers. We communicate closely with customers to establish their quality requirements. Consistent Quality Our plant has strict quality control in each manufacturin
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inquirycas 915087-33-1 99 % purity Enzalutamide powder Product Name: Enzalutamide CAS: 915087-33-1 MF: C21H16F4N4O2S MW: 464.44 EINECS: 805-022-1 Appearance:white Storage:room Package:drum Application:Artemisia annua is used as antima
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Cas:915087-33-1
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Cas:915087-33-1
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Cas:915087-33-1
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inquiryEnzalutamide CAS: 915087-33-1 Specification Chemical Name enzalutamide Synonyms MDV 3100;XTANDI;UNII-93T0T9GKNU;[14C]-Enzalutamide;N-methyl-4-[3-(4-cyano-3-trifluoromethylphenyl)-5,5-dimethyl-4-oxo-2-thioxoimidazolidi
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Type:Trading Company
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Cas:915087-33-1
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inquiry4-isothiocyanato 2-(trifluoromethyl)benzonitrile
enzalutamide
Conditions | Yield |
---|---|
In dimethyl sulfoxide at 80℃; for 4h; Concentration; Temperature; Edman Degradation; | 90.9% |
In Isopropyl acetate at 75 - 85℃; for 8h; | 557 g |
4-isothiocyanato 2-(trifluoromethyl)benzonitrile
enzalutamide
Conditions | Yield |
---|---|
In Isopropyl acetate; dimethyl sulfoxide at 85℃; for 16h; | 90.3% |
4-bromo-2-fluoro-N-methylbenzanamide
2-(trifluoromethyl)-4-(4,4-dimethyl 5-oxo-2-thioimidazolin-1-yl)benzonitrile
enzalutamide
Conditions | Yield |
---|---|
With copper(l) iodide; 2-acetylcyclohexanone; potassium carbonate In N,N-dimethyl-formamide at 110℃; for 22h; Inert atmosphere; | 88.7% |
Stage #1: 2-(trifluoromethyl)-4-(4,4-dimethyl 5-oxo-2-thioimidazolin-1-yl)benzonitrile With sodium hydride In N,N-dimethyl-formamide at 0 - 5℃; for 0.5h; Stage #2: 4-bromo-2-fluoro-N-methylbenzanamide In N,N-dimethyl-formamide at 0 - 20℃; for 5h; | 87.3% |
2-((3-fluoro-4-(methylcarbamoyl)phenyl)amino)-2-methyl propanoic acid
4-isothiocyanato 2-(trifluoromethyl)benzonitrile
enzalutamide
Conditions | Yield |
---|---|
Stage #1: 2-((3-fluoro-4-(methylcarbamoyl)phenyl)amino)-2-methyl propanoic acid With triethylamine In dichloromethane; toluene at 30℃; for 0.166667h; Stage #2: 4-isothiocyanato 2-(trifluoromethyl)benzonitrile In toluene at 50 - 60℃; for 4h; Temperature; Solvent; | 88.5% |
With N-ethyl-N,N-diisopropylamine; phenol at 60℃; for 4h; Reagent/catalyst; | 77% |
Stage #1: 4-isothiocyanato 2-(trifluoromethyl)benzonitrile With triethylamine In chloroform at 20℃; for 0.25h; Reflux; Inert atmosphere; Stage #2: 2-((3-fluoro-4-(methylcarbamoyl)phenyl)amino)-2-methyl propanoic acid In chloroform for 6h; Reagent/catalyst; Reflux; | 76.92% |
Conditions | Yield |
---|---|
In tetrahydrofuran; water at -13℃; for 5h; | 88.18% |
In toluene at 50℃; for 0.5h; Solvent; Temperature; | 86% |
In tetrahydrofuran; water at -11 - -7℃; for 22.6667h; Temperature; Large scale; | 83.6% |
4-isothiocyanato 2-(trifluoromethyl)benzonitrile
enzalutamide
Conditions | Yield |
---|---|
In Isopropyl acetate; dimethyl sulfoxide at 80℃; for 6h; Temperature; | 88% |
With Isopropyl acetate In dimethyl sulfoxide at 90 - 95℃; | 0.2 g |
In Isopropyl acetate; dimethyl sulfoxide at 90 - 95℃; | 0.2 g |
4-isothiocyanato 2-(trifluoromethyl)benzonitrile
enzalutamide
Conditions | Yield |
---|---|
In Isopropyl acetate; dimethyl sulfoxide at 85℃; for 6h; Temperature; | 88% |
In dimethyl sulfoxide at 84℃; for 4h; Edman Degradation; | 86% |
With copper(l) iodide; potassium carbonate In dimethyl sulfoxide at 80℃; Bucherer-Bergs Reaction; Inert atmosphere; | 309 g |
2-(3-fluoro-4-(methylcarbamoyl)phenylamino)-2-methylpropanoic acid methyl ester
4-isothiocyanato 2-(trifluoromethyl)benzonitrile
enzalutamide
Conditions | Yield |
---|---|
In Isopropyl acetate; dimethyl sulfoxide at 70℃; for 6h; Temperature; | 85% |
In Isopropyl acetate; dimethyl sulfoxide at 83 - 84℃; for 17.5h; | 82% |
In Isopropyl acetate; dimethyl sulfoxide at 55 - 85℃; Inert atmosphere; | 80.2% |
4-isothiocyanato 2-(trifluoromethyl)benzonitrile
enzalutamide
Conditions | Yield |
---|---|
Edman Degradation; | 85% |
Conditions | Yield |
---|---|
In Isopropyl acetate; dimethyl sulfoxide at 80 - 85℃; | 83% |
4-isothiocyanato 2-(trifluoromethyl)benzonitrile
enzalutamide
Conditions | Yield |
---|---|
In dimethyl sulfoxide at 84℃; for 4h; Concentration; Temperature; Edman Degradation; | 82% |
Conditions | Yield |
---|---|
In Isopropyl acetate; dimethyl sulfoxide at 80 - 85℃; for 20h; | 82% |
methyl 2-chloroisobutyrate
enzalutamide
Conditions | Yield |
---|---|
With triethylamine In N,N-dimethyl-formamide at 80 - 90℃; for 5h; | 66.4% |
Conditions | Yield |
---|---|
In acetonitrile at 20 - 70℃; for 64h; Molecular sieve; Inert atmosphere; | 47.3% |
N-methyl-2-fluoro-4-(1,1-dimethyl-cyanomethyl)-aminobenzamide
thiophosgene
4-amino-2-trifluoromethylbenzonitrile
enzalutamide
Conditions | Yield |
---|---|
Stage #1: N-methyl-2-fluoro-4-(1,1-dimethyl-cyanomethyl)-aminobenzamide; thiophosgene; 4-amino-2-trifluoromethylbenzonitrile In N,N-dimethyl acetamide at 0 - 60℃; Inert atmosphere; Stage #2: With hydrogenchloride In methanol; N,N-dimethyl acetamide for 2h; Inert atmosphere; Reflux; | 41% |
N-methyl-2-fluoro-4-(1,1-dimethyl-cyanomethyl)-aminobenzamide
4-isothiocyanato 2-(trifluoromethyl)benzonitrile
enzalutamide
Conditions | Yield |
---|---|
Stage #1: N-methyl-2-fluoro-4-(1,1-dimethyl-cyanomethyl)-aminobenzamide; 4-isothiocyanato 2-(trifluoromethyl)benzonitrile In N,N-dimethyl-formamide at 100℃; for 11h; Microwave irradiation; Stage #2: With hydrogenchloride In methanol; N,N-dimethyl-formamide for 1.5h; Heating / reflux; | 25% |
Stage #1: N-methyl-2-fluoro-4-(1,1-dimethyl-cyanomethyl)-aminobenzamide; 4-isothiocyanato 2-(trifluoromethyl)benzonitrile In N,N-dimethyl-formamide at 100℃; for 11h; Microwave irradiation; Stage #2: With hydrogenchloride; methanol In water; N,N-dimethyl-formamide for 1h; Reflux; | 23.1% |
Stage #1: N-methyl-2-fluoro-4-(1,1-dimethyl-cyanomethyl)-aminobenzamide; 4-isothiocyanato 2-(trifluoromethyl)benzonitrile In N,N-dimethyl-formamide at 120℃; for 16h; Stage #2: With hydrogenchloride; water In ethanol; N,N-dimethyl-formamide for 1h; Reflux; | 17.1% |
4-[1-(4-cyano-3-trifluoromethyl-phenylcarbamoyl)-1-methyl-ethylamino]-2-fluoro-N-methyl-benzamide
enzalutamide
Conditions | Yield |
---|---|
With dmap; thiophosgene In acetonitrile at 40 - 60℃; for 24h; Solvent; Reagent/catalyst; Temperature; Inert atmosphere; | 19.1% |
thiophosgene
4-[1-(4-cyano-3-trifluoromethyl-phenylcarbamoyl)-1-methyl-ethylamino]-2-fluoro-N-methyl-benzamide
enzalutamide
Conditions | Yield |
---|---|
at 100℃; for 6h; a sealed-tube; | 4% |
at 100℃; for 6h; Sealed tube; | 1.5% |
enzalutamide
Conditions | Yield |
---|---|
With hydrogenchloride; water In methanol; N,N-dimethyl-formamide for 1.5h; Heating / reflux; | |
With hydrogenchloride; water In methanol; N,N-dimethyl-formamide for 1.5h; Reflux; Inert atmosphere; | 30 mg |
2-fluoro-4-bromobenzoic acid
enzalutamide
Conditions | Yield |
---|---|
Multi-step reaction with 5 steps 1.1: thionyl chloride / N,N-dimethyl-formamide; Isopropyl acetate / 4.58 h / 21 - 72 °C / Inert atmosphere; Industry scale 2.1: water; Isopropyl acetate / 1.08 h / 2 - 35 °C / Inert atmosphere; Industry scale 3.1: potassium carbonate / copper(l) chloride / N,N-dimethyl-formamide; water / 30 °C 3.2: 105 °C / Inert atmosphere 3.3: pH 4 4.1: potassium carbonate / N,N-dimethyl-formamide; water / 30 °C 4.2: 1.08 h / 32 - 40 °C 5.1: dimethyl sulfoxide; Isopropyl acetate / 17.5 h / 83 - 84 °C View Scheme | |
Multi-step reaction with 5 steps 1.1: thionyl chloride / N,N-dimethyl-formamide; Isopropyl acetate / 4.58 h / 21 - 72 °C / Inert atmosphere; Industry scale 2.1: water; Isopropyl acetate / 1.08 h / 2 - 35 °C / Inert atmosphere; Industry scale 3.1: potassium carbonate / copper(l) chloride / N,N-dimethyl-formamide; water / 30 °C 3.2: 105 °C / Inert atmosphere 3.3: pH 4 4.1: 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride / dichloromethane / 20 °C 5.1: 6 h / 100 °C / a sealed-tube View Scheme | |
Multi-step reaction with 4 steps 1.1: N,N-dimethyl-formamide; oxalyl dichloride / dichloromethane / 10 - 30 °C 2.1: water; tert-butyl methyl ether / 10 - 30 °C / pH 8 - 9 3.1: potassium carbonate / N,N-dimethyl-formamide; 1,4-dioxane; water / 0.33 h / Inert atmosphere 3.2: 24.33 h / Inert atmosphere; Reflux 4.1: triethylamine / dichloromethane / 23 - 28 °C / Inert atmosphere View Scheme |
4-bromo-2-fluorobenzoyl chloride
enzalutamide
Conditions | Yield |
---|---|
Multi-step reaction with 4 steps 1.1: water; Isopropyl acetate / 1.08 h / 2 - 35 °C / Inert atmosphere; Industry scale 2.1: potassium carbonate / copper(l) chloride / N,N-dimethyl-formamide; water / 30 °C 2.2: 105 °C / Inert atmosphere 2.3: pH 4 3.1: potassium carbonate / N,N-dimethyl-formamide; water / 30 °C 3.2: 1.08 h / 32 - 40 °C 4.1: dimethyl sulfoxide; Isopropyl acetate / 17.5 h / 83 - 84 °C View Scheme | |
Multi-step reaction with 4 steps 1.1: water; Isopropyl acetate / 1.08 h / 2 - 35 °C / Inert atmosphere; Industry scale 2.1: potassium carbonate / copper(l) chloride / N,N-dimethyl-formamide; water / 30 °C 2.2: 105 °C / Inert atmosphere 2.3: pH 4 3.1: 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride / dichloromethane / 20 °C 4.1: 6 h / 100 °C / a sealed-tube View Scheme | |
Multi-step reaction with 3 steps 1.1: water; tert-butyl methyl ether / 10 - 30 °C / pH 8 - 9 2.1: potassium carbonate / N,N-dimethyl-formamide; 1,4-dioxane; water / 0.33 h / Inert atmosphere 2.2: 24.33 h / Inert atmosphere; Reflux 3.1: triethylamine / dichloromethane / 23 - 28 °C / Inert atmosphere View Scheme |
4-amino-2-trifluoromethylbenzonitrile
enzalutamide
Conditions | Yield |
---|---|
Multi-step reaction with 2 steps 1: n-heptane; water / 16.5 h / 5 - 46.4 °C / Industry scale; Inert atmosphere 2: dimethyl sulfoxide; Isopropyl acetate / 17.5 h / 83 - 84 °C View Scheme | |
Multi-step reaction with 2 steps 1.1: water / 1 h / 20 °C 2.1: N,N-dimethyl-formamide / 16 h / 120 °C 2.2: 1 h / Reflux View Scheme | |
Multi-step reaction with 2 steps 1.1: dichloromethane; water / 0.25 h / 20 - 30 °C / Inert atmosphere 1.2: 4 h 2.1: triethylamine / chloroform / 0.25 h / 20 °C / Reflux; Inert atmosphere 2.2: 6 h / Reflux View Scheme |
4-bromo-2-fluoro-N-methylbenzanamide
enzalutamide
Conditions | Yield |
---|---|
Multi-step reaction with 3 steps 1.1: potassium carbonate / copper(l) chloride / N,N-dimethyl-formamide; water / 30 °C 1.2: 105 °C / Inert atmosphere 1.3: pH 4 2.1: potassium carbonate / N,N-dimethyl-formamide; water / 30 °C 2.2: 1.08 h / 32 - 40 °C 3.1: dimethyl sulfoxide; Isopropyl acetate / 17.5 h / 83 - 84 °C View Scheme | |
Multi-step reaction with 3 steps 1.1: potassium carbonate / copper(l) chloride / N,N-dimethyl-formamide; water / 30 °C 1.2: 105 °C / Inert atmosphere 1.3: pH 4 2.1: 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride / dichloromethane / 20 °C 3.1: 6 h / 100 °C / a sealed-tube View Scheme | |
Multi-step reaction with 2 steps 1.1: potassium carbonate / N,N-dimethyl-formamide; 1,4-dioxane; water / 0.33 h / Inert atmosphere 1.2: 24.33 h / Inert atmosphere; Reflux 2.1: triethylamine / dichloromethane / 23 - 28 °C / Inert atmosphere View Scheme |
2-((3-fluoro-4-(methylcarbamoyl)phenyl)amino)-2-methyl propanoic acid
enzalutamide
Conditions | Yield |
---|---|
Multi-step reaction with 2 steps 1.1: potassium carbonate / N,N-dimethyl-formamide; water / 30 °C 1.2: 1.08 h / 32 - 40 °C 2.1: dimethyl sulfoxide; Isopropyl acetate / 17.5 h / 83 - 84 °C View Scheme | |
Multi-step reaction with 2 steps 1: 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride / dichloromethane / 20 °C 2: 6 h / 100 °C / a sealed-tube View Scheme | |
Multi-step reaction with 2 steps 1: potassium carbonate / N,N-dimethyl-formamide / 10 h / 50 °C 2: dimethyl sulfoxide / 4 h / 84 °C View Scheme |
2-fluoro-4-nitrobenzoic acid
enzalutamide
Conditions | Yield |
---|---|
Multi-step reaction with 4 steps 1.1: 1,1'-carbonyldiimidazole / dichloromethane / 1 h / 20 °C 1.2: 1 h 2.1: acetic acid; iron / ethyl acetate / 16 h / Reflux 3.1: acetic acid / 16 h / 80 °C / Sealed tube 4.1: N,N-dimethyl-formamide / 16 h / 120 °C 4.2: 1 h / Reflux View Scheme | |
Multi-step reaction with 4 steps 1: benzotriazol-1-ol; 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride; triethylamine / dichloromethane / 5.5 h / 0 - 25 °C 2: palladium 10% on activated carbon; hydrogen / methanol / 27 °C / 1500.15 - 1875.19 Torr 3: N-ethyl-N,N-diisopropylamine; tetra-(n-butyl)ammonium iodide / tetrahydrofuran / 8 h / 80 - 85 °C 4: Isopropyl acetate / dimethyl sulfoxide / 90 - 95 °C View Scheme | |
Multi-step reaction with 5 steps 1.1: N,N-dimethyl-formamide; thionyl chloride / Isopropyl acetate / 60 °C / Inert atmosphere 2.1: Isopropyl acetate / 5 h / Inert atmosphere 3.1: hydrogen; palladium 10% on activated carbon / methanol / 1 h / 50 °C / 4500.45 Torr / Autoclave 3.2: Heating 4.1: triethylamine / N,N-dimethyl acetamide / 1 h / 70 °C 4.2: 1.67 h / 100 °C 5.1: N-ethyl-N,N-diisopropylamine; phenol / 4 h / 60 °C View Scheme |
2-fluoro-N-methyl-4-nitro-benzamide
enzalutamide
Conditions | Yield |
---|---|
Multi-step reaction with 3 steps 1.1: acetic acid; iron / ethyl acetate / 16 h / Reflux 2.1: acetic acid / 16 h / 80 °C / Sealed tube 3.1: N,N-dimethyl-formamide / 16 h / 120 °C 3.2: 1 h / Reflux View Scheme | |
Multi-step reaction with 3 steps 1: palladium 10% on activated carbon; hydrogen / methanol / 27 °C / 1500.15 - 1875.19 Torr 2: N-ethyl-N,N-diisopropylamine; tetra-(n-butyl)ammonium iodide / tetrahydrofuran / 8 h / 80 - 85 °C 3: Isopropyl acetate / dimethyl sulfoxide / 90 - 95 °C View Scheme | |
Multi-step reaction with 3 steps 1.1: hydrogen; palladium 10% on activated carbon / methanol / 1 h / 50 °C / 4500.45 Torr / Autoclave 1.2: Heating 2.1: triethylamine / N,N-dimethyl acetamide / 1 h / 70 °C 2.2: 1.67 h / 100 °C 3.1: N-ethyl-N,N-diisopropylamine; phenol / 4 h / 60 °C View Scheme |
2-fluoro-N-methyl-4-amino-benzamide
enzalutamide
Conditions | Yield |
---|---|
Multi-step reaction with 2 steps 1.1: acetic acid / 16 h / 80 °C / Sealed tube 2.1: N,N-dimethyl-formamide / 16 h / 120 °C 2.2: 1 h / Reflux View Scheme | |
Multi-step reaction with 2 steps 1: N-ethyl-N,N-diisopropylamine; tetra-(n-butyl)ammonium iodide / tetrahydrofuran / 8 h / 80 - 85 °C 2: Isopropyl acetate / dimethyl sulfoxide / 90 - 95 °C View Scheme | |
Multi-step reaction with 2 steps 1: acetic acid / acetone / 85 °C 2: pyridine / 60 - 90 °C View Scheme |
2-fluoro-4-nitrotoluene
enzalutamide
Conditions | Yield |
---|---|
Multi-step reaction with 5 steps 1.1: sodium bromide; sulfuric acid / water / 80 - 85 °C 1.2: 27 h / 80 - 85 °C 2.1: benzotriazol-1-ol; 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride; triethylamine / dichloromethane / 5.5 h / 0 - 25 °C 3.1: palladium 10% on activated carbon; hydrogen / methanol / 27 °C / 1500.15 - 1875.19 Torr 4.1: N-ethyl-N,N-diisopropylamine; tetra-(n-butyl)ammonium iodide / tetrahydrofuran / 8 h / 80 - 85 °C 5.1: Isopropyl acetate / dimethyl sulfoxide / 90 - 95 °C View Scheme | |
Multi-step reaction with 5 steps 1.1: periodic acid; chromium(VI) oxide / acetonitrile / 1 h 2.1: thionyl chloride / N,N-dimethyl-formamide / 1 h / -5 °C 2.2: 1 h 3.1: acetic acid; iron / ethyl acetate / 1 h / Reflux 4.1: magnesium sulfate / 12 h / 80 °C 5.1: N,N-dimethyl acetamide / 100 °C 5.2: 1.5 h / Reflux View Scheme |
enzalutamide
Conditions | Yield |
---|---|
Multi-step reaction with 2 steps 1.1: triethylamine / N,N-dimethyl acetamide / 1 h / 70 °C 1.2: 1.67 h / 100 °C 2.1: N-ethyl-N,N-diisopropylamine; phenol / 4 h / 60 °C View Scheme |
2-fluoro-4-nitrobenzoyl chloride
enzalutamide
Conditions | Yield |
---|---|
Multi-step reaction with 4 steps 1.1: Isopropyl acetate / 5 h / Inert atmosphere 2.1: hydrogen; palladium 10% on activated carbon / methanol / 1 h / 50 °C / 4500.45 Torr / Autoclave 2.2: Heating 3.1: triethylamine / N,N-dimethyl acetamide / 1 h / 70 °C 3.2: 1.67 h / 100 °C 4.1: N-ethyl-N,N-diisopropylamine; phenol / 4 h / 60 °C View Scheme |
enzalutamide
4-(3-(4-cyano-3-(trifluoromethyl)phenyl)-5,5-dimethyl-4-oxo-2-imidazolidinethione-1-yl)-2-fluorobenzoic acid
Conditions | Yield |
---|---|
With hydrogenchloride In 1,4-dioxane for 2h; Reflux; | 95% |
With hydrogenchloride In 1,4-dioxane; water for 2h; Reflux; | 95% |
With hydrogenchloride In water at 120℃; for 48h; Pressure vessel; | |
With hydrogenchloride In water at 120℃; for 48h; |
enzalutamide
di-tert-butyl dicarbonate
Conditions | Yield |
---|---|
With dmap In dichloromethane at 25℃; for 12h; | 92.3% |
enzalutamide
tetramethylammonium fluoride
Conditions | Yield |
---|---|
In toluene at 100℃; for 12h; | 53% |
enzalutamide
Conditions | Yield |
---|---|
With 2,2,6,6-tetramethyl-piperidine; 1,2,2,6,6-pentamethylpiperidine; 4-sulfanylphenol; 1,3-dicyano-2,4,5,6-tetrakis(N,N-diphenylamino)-benzene In 1,2-dichloro-ethane at 25℃; for 12h; Sealed tube; Irradiation; Inert atmosphere; | 40% |
enzalutamide
bis(trichloromethyl) carbonate
Conditions | Yield |
---|---|
Stage #1: enzalutamide With chloro-trimethyl-silane; triethylamine In tetrahydrofuran at 60℃; for 0.5h; Cooling with ice; Stage #2: bis(trichloromethyl) carbonate In tetrahydrofuran at 60℃; for 2h; Stage #3: isopropyl (2S)-2-[[[4-(hydroxymethyl)phenoxy](methoxymethyl)phosphoryl]amino]propanoate With dmap In tetrahydrofuran at 20℃; for 1h; Cooling with ice; | 27.76% |
Conditions | Yield |
---|---|
With C10H12O2NiC8H12-1,5-cyclo; triphenylborane; diphenyl(methyl)phosphine In 1-methyl-pyrrolidin-2-one at 100℃; for 18h; Inert atmosphere; Glovebox; Sealed tube; | 13% |
enzalutamide
4-(3-(4-cyano-3-(trifluoromethyl)phenyl)-5,5-dimethyl-2,4-dioxoimidazolidin-1-yl)-2-fluoro-N-methylbenzamide
Conditions | Yield |
---|---|
With dihydrogen peroxide In ethanol; water for 1h; Reflux; |
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